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Astemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice. Structure.
Cytochrome p450 3A4. My understanding is that Astemizole is a prodrug, which is expected to be metabolised into its active metabolite by first-pass hepatic metabolism; the prodrug is cardiotoxic, leading to an increased QTc on overdoes or when administered to a patient with impaired 3A4 activity.